{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,10,13]],"date-time":"2026-10-13T04:46:50Z","timestamp":1791866810258,"version":"4.3.4"},"reference-count":108,"publisher":"MDPI AG","issue":"19","license":[{"start":{"date-parts":[[2026,10,6]],"date-time":"2026-10-06T00:00:00Z","timestamp":1791244800000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"},{"start":{"date-parts":[[2026,10,6]],"date-time":"2026-10-06T00:00:00Z","timestamp":1791244800000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Int. J. Mol. Sci.","IJMS"],"abstract":"<jats:p>Angiotensin receptor blockers (ARBs), also known as sartans, are a family of highly selective angiotensin II type 1 receptor antagonists commonly prescribed to individuals with hypertension, heart failure, and chronic kidney disease. Additionally, the discovery and facile synthesis of bisartans, a novel class of ARB antihypertensives, have shown therapeutic promise for cardiovascular diseases. Recent computational and network pharmacology studies have shown a broader receptor interactome, encompassing alpha-adrenergic receptors, and delta- and mu-opioid receptors, highlighting the polypharmacology of ARBs. Herein, we combine molecular docking, molecular dynamics, and protein\u2013protein interaction analyses to characterize the binding profiles of sartans and bisartans, as well as conformational impacts across multiple G-protein-coupled receptors. Emphasis is placed on their potential to modulate receptor desensitization states and influence pathways involved in neuropsychiatric disorders, addiction, viral infections, and cardiovascular diseases. Limitations of current computational approaches are discussed alongside the need for experimental proteomic validation. Collectively, this evidence positions sartans and bisartans as structurally privileged scaffolds for multi-target drug repurposing and precision medicine applications.<\/jats:p>","DOI":"10.3390\/ijms27198883","type":"journal-article","created":{"date-parts":[[2026,10,6]],"date-time":"2026-10-06T14:28:05Z","timestamp":1791296885000},"page":"8883","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":0,"title":["Sartans and Bisartans: Expanding Therapeutic Horizons Through Broad Receptor Interactions and Repurposing Potential"],"prefix":"10.3390","volume":"27","author":[{"ORCID":"https:\/\/orcid.org\/0009-0001-3805-6558","authenticated-orcid":false,"given":"Errikos","family":"Petsas","sequence":"first","affiliation":[{"name":"Laboratory of Organic Chemistry, Department of Chemistry, National and Kapodistrian University of Athens, 15771 Athens, Greece"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-6788-2771","authenticated-orcid":false,"given":"Vasso","family":"Apostolopoulos","sequence":"additional","affiliation":[{"name":"School of Health and Biomedical Sciences, RMIT University, Melbourne, VIC 3000, Australia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0009-0004-5104-8044","authenticated-orcid":false,"given":"Despoina P.","family":"Kiouri","sequence":"additional","affiliation":[{"name":"Laboratory of Organic Chemistry, Department of Chemistry, National and Kapodistrian University of Athens, 15771 Athens, Greece"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Konstantinos","family":"Kelaidonis","sequence":"additional","affiliation":[{"name":"NewDrug PC, Patras Science Park, 26504 Patras, Greece"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Harry","family":"Ridgway","sequence":"additional","affiliation":[{"name":"THERAmolecular, LLC., Rodeo, NM 88056, USA"},{"name":"Institute for Sustainable Industries and Liveable Cities, Victoria University, Melbourne, VIC 8001, Australia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Graham J.","family":"Moore","sequence":"additional","affiliation":[{"name":"Pepmetics Inc., 772 Murphy Place, Victoria, BC V8Y 3H4, Canada"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-5309-992X","authenticated-orcid":false,"given":"Thomas","family":"Mavromoustakos","sequence":"additional","affiliation":[{"name":"Laboratory of Organic Chemistry, Department of Chemistry, National and Kapodistrian University of Athens, 15771 Athens, Greece"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-4801-8061","authenticated-orcid":false,"given":"Laura Kate","family":"Gadanec","sequence":"additional","affiliation":[{"name":"Institute for Health and Sport, Victoria University, Melbourne, VIC 3030, Australia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"John M.","family":"Matsoukas","sequence":"additional","affiliation":[{"name":"NewDrug PC, Patras Science Park, 26504 Patras, Greece"},{"name":"Institute for Health and Sport, Victoria University, Melbourne, VIC 3030, Australia"},{"name":"Department of Chemistry, University of Patras, 26504 Patras, Greece"},{"name":"Department of Physiology and Pharmacology, Cumming School of Medicine, University of Calgary, Calgary, AB T2N 1N4, Canada"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-8728-6245","authenticated-orcid":false,"given":"Christos T.","family":"Chasapis","sequence":"additional","affiliation":[{"name":"Laboratory of Organic Chemistry, Department of Chemistry, National and Kapodistrian University of Athens, 15771 Athens, Greece"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"1968","published-online":{"date-parts":[[2026,10,6]]},"reference":[{"key":"ref_1","doi-asserted-by":"crossref","first-page":"3627","DOI":"10.1093\/eurheartj\/ehad195","article-title":"2023 focused update of the 2021 ESC guidelines for the diagnosis and treatment of acute and chronic heart failure: Developed by the task force for the diagnosis and treatment of acute and chronic heart failure of the European Society of Cardiology (ESC) with the special contribution of the Heart Failure Association (HFA) of the ESC","volume":"44","author":"McDonagh","year":"2023","journal-title":"Eur. 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